Zeposia
Ozanimod
Relapsing forms of Multiple Sclerosis (MS)
Moderately to severely active Ulcerative Colitis (UC)
Oral disease-modifying therapy (DMT), sphingosine 1-phosphatase receptor modulator
Capsule
By mouth
Zeposia has labeled indications for the treatment of relapsing forms of multiple sclerosis (MS) in adults, including clinically isolated syndrome, relapsing-remitting diseases, and active progressive disease. It is also FDA-approved for the treatment of moderately to severely active ulcerative colitis in adults.
Prior to initiating therapy with Zeposia, patients will have baseline lab work to evaluate their immune status and liver function, a varicella serology to determine the need for vaccination, an electrocardiogram to obtain baseline parameters (and, in those with a history of pre-existing heart conditions, may require a more in-depth cardiology evaluation), and an ophthalmologic examination in patients with a history of uveitis or macular edema.
Zeposia doses should be titrated over seven days to reduce the development of bradycardia or slowed heart rate. Given the risk of decreased heart rate, Zeposia should be avoided with QT-prolonging drugs and heart rate-lowering medications, like beta-blockers.
Zeposia can cause serious side effects, such as an increased risk of infections caused by viruses, fungi, or bacteria. Zeposia use comes with the potential to develop two serious conditions: progressive multifocal leukoencephalopathy (PML) and posterior reversible encephalopathy syndrome (PRES).
Live vaccines are not recommended during therapy and should be given at least four weeks prior to initiation or held for three months after discontinuation of Zeposia. Prior to initiation of Zeposia, your antibodies to certain vaccine-preventable diseases, such as varicella-zoster virus, may be checked to determine the need for (re)vaccination.
Zeposia is contraindicated in patients who, during the prior six months, have had a myocardial infarction, stroke, unstable angina, transient ischemic attack, decompensated heart failure requiring hospitalization, or Class III/IV heart failure.
Consumption of Zeposia with foods and beverages with high tyramine content may cause sudden and severe high blood pressure, so concurrent ingestion should be avoided. The risk of a hypertensive emergency is also why Zeposia should not be taken with monoamine oxidase inhibitors (MAOIs).
Zeposia capsule
Ozanimod 0.92 mg
Zeposia starter kit
Ozanimod 0.23 mg (4 capsules), ozanimod 0.46 mg (3 capsules), and ozanimod 0.92 mg (21 capsules)
Zeposia 7-day starter kit
Ozanimod 0.23 mg (4 capsules) and ozanimod 0.46 mg (3 capsules)
Relapsing multiple sclerosis
Initial: 0.23 mg once daily on days 1 through 4, then 0.46 mg once daily on days 5 through 7
Maintenance: 0.92 mg once daily starting on day 8
Ulcerative colitis
Initial: 0.23 mg once daily on days 1 through 4, then 0.46 mg once daily on days 5 through 7
Maintenance: 0.92 mg once daily starting on day 8
Zeposia is titrated slowly over the first week of therapy. The recommended starting dose of Zeposia is 0.23 mg by mouth once daily on days 1 through 4, then 0.46 mg by mouth once daily on days 5 through 7, and finally 0.92 mg by mouth once daily on day 8 and thereafter.
Zeposia capsules should be swallowed whole and can be taken with or without food.
If you miss a dose of Zeposia, take it as soon as you remember. However, if it’s close to the time of your next dose, do not double up doses to make up for the missed dose. Take the next scheduled dose and resume daily doses.
Abruptly stopping Zeposia, more than just a dose or two, may be associated with rebound MS in some MS patients; completely stopping this medication should always be done under the supervision of a medical professional.
Zeposia is not right for everyone. This medication should not be used in individuals with a recent history (within the past 6 months) of myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or class III/IV heart failure. In individuals with certain types of atrioventricular heart block, sick sinus syndrome, or sinoatrial block. Zeposia should also be avoided unless the individual has a functional pacemaker.
Zeposia is contraindicated in those with severe untreated sleep apnea, given the risk of reduced pulmonary function while on therapy, and those taking monoamine oxidase inhibitors, given the additive risk of dangerously high blood pressure.
This medicine increases the risk of infection by suppressing the immune system. Initiation should be postponed in patients with active infections, and patients should be tested for immunity to varicella zoster virus (VZV) if they do not have a history of varicella (chickenpox) or have not received a full vaccine regimen against VZV.
Given the immune suppression associated with Zeposia, live-attenuated vaccines should be administered at least one month prior to Zeposia administration. Such vaccines should be avoided during treatment and held until 3 months after completion of the medication.
Zeposia should be avoided in patients with a significant cardiac history, including those with certain arrhythmias requiring treatment with certain medications, ischemic heart disease, heart failure, uncontrolled hypertension, and a recent history of myocardial infarction, among other conditions. Patients with a cardiac history should be reviewed by a cardiologist to evaluate the appropriateness of receiving Zeposia.
Zeposia is not recommended in patients with liver disease.
This medication is associated with an increased risk of cancer, including rectal adenocarcinoma and malignant neoplasm of the breast, but particularly basal cell carcinoma of the skin and malignant melanoma. Limiting exposure to sunlight, wearing protective clothing, and applying regular sunscreen with a high sun protection factor (SPF) is important while on Zeposia.
Zeposia can lower your immune system, so it should be spaced out from live vaccines.
Zeposia should not be taken cautiously with other medications that may suppress the immune system, and ideally, concomitant use should be avoided altogether. The immune system should recover within 3 months after stopping Zeposia.
Some medications can affect how Zeposia works or can increase the side effects associated with its use. Tell your doctor if you are taking any of the following: MAOIs, CYP2C8 inhibitors or inducers, breast cancer resistance (BRCP) inhibitors, any medication that can increase serotonin or norepinephrine (e.g., opioids, SSRIs, or SNRIs). Zeposia should also not be taken with QT-prolonging medications or medications that slow the heart rate, such as beta-blockers.
Any new or worsening medical problems should be reported to a provider immediately, especially a decrease in heart rate. Headaches, confusion, vision problems, seizures, or any stroke-like symptoms warrant a trip to the emergency room for immediate intervention.
Serious side effects:
Headache, seizures, confusion, aphasia
Blurred vision
Bradycardia
High blood pressure
Less serious side effects:
Upper respiratory infection
Liver enzyme changes
Orthostatic hypotension
Urinary tract infection
Upper abdominal pain
Decreased circulating lymphocytes
Types of Multiple Sclerosis, National Multiple Sclerosis Society (2024)
A case of posterior reversible encephalopathy syndrome associated with Gilenya® (fingolimod) treatment for multiple sclerosis, Frontiers in Neurology (2015)
Uveitis, Mayo Clinic (2023)
Macular Edema, National Eye Institute (2023)
Disease reactivation after cessation of disease-modifying therapy in patients with relapsing-remitting multiple sclerosis, Neurology (2023)
Drug development and drug interactions: table of substrates, inhibitors, and inducers, U.S. Food and Drug Administration (2023)
Novel inhibitors of breast cancer resistance protein (BRCP, ABCG2) among marketed drugs, European Journal of Pharmaceutical Sciences (2023)
S1P receptor modulators in Multiple Sclerosis: detecting a potential skin cancer safety signal, Multiple Sclerosis and Related Disorders (2022)
Sphingosine-1 phosphatase receptor modulators increase in vitro melanoma cell line proliferation at therapeutic doses used in patients with multiple sclerosis, Neurology and Therapy (2023)
Marissa Walsh, Pharm.D., BCPS-AQ ID, graduated with her Doctor of Pharmacy degree from the University of Rhode Island in 2009, then went on to complete a PGY1 Pharmacy Practice Residency at Charleston Area Medical Center in Charleston, West Virginia, and a PGY2 Infectious Diseases Pharmacy Residency at Maine Medical Center in Portland, Maine. Dr. Walsh has worked as a clinical pharmacy specialist in Infectious Diseases in Portland, Maine, and Miami, Florida, prior to setting into her current role in Buffalo, New York, where she continues to work as an Infectious Diseases Pharmacist in a hematology/oncology population.
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